[CAS NO. 1297538-32-9] Darolutamide (ODM-201)

Name: Darolutamide (ODM-201)
Brand: Arctom Scientific
SKU: SLK-S7559

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PRODUCTS SPECIFICATIONS [1297538-32-9]

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Catalog

SLK-S7559

Brand

Selleck

CAS

1297538-32-9

DESCRIPTION [1297538-32-9]

Overview

MDL	MFCD29472270
Molecular Weight	398.85
Molecular Formula	C19H19ClN6O2
SMILES	C([C@@H](NC(=O)C=1C=C(C(C)O)NN1)C)N2N=C(C=C2)C3=CC(Cl)=C(C#N)C=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5072 mL	12.5360 mL	25.0721 mL
5 mM	0.5014 mL	2.5072 mL	5.0144 mL
10 mM	0.2507 mL	1.2536 mL	2.5072 mL
50 mM	0.0501 mL	0.2507 mL	0.5014 mL

Description

Darolutamide (ODM-201, BAY-1841788) is a novel (AR) antagonist that blocks AR nuclear translocation with of 11 nM. Phase 3.

Targets

Androgen receptor ^[1]

11 nM(Ki)

In vitro

In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells.

In vivo

In mice bearing VCaP xenografts, ODM-201 (50 mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth.

References

[1] Moilanen AM, et al. Sci Rep. 2015, 5:12007. doi: 10.1038/srep12007.

Synonyms

1H-Pyrazole-3-carboxamide, N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-

N-[(1S)-2-[3-(3-Chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide

Darolutamide

ODM 201

BAY 1841788

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